Podophyllotoxin and 4′-demethylepipodophyllotoxin are precursor compounds with unique anti-tumor natural activity, extracted from podophylloideae plants (such as Berberidaceae Sinopodophyllum hexandrum, umbrellaleaf, dysosma versipellis etc.). However, podophyllotoxin or 4′-demethylepipodophyllotoxin has more or less shortcomings to be overcome, such as strong toxic and side effect and poor bioavailability, thus limiting their clinical application.